Takeda Pharmaceutical Company Limited.
Clin Pharmacol Drug Dev. 2018 Mar;7(3):319-331. doi: 10.1002/cpdd.381. Epub 2017 Sep 21.
Three phase 1 randomized single-center studies assessed the pharmacokinetics, safety, and tolerability of vortioxetine after single- and multiple-dose administration in healthy Japanese adults. Study 1 assessed the pharmacokinetics of vortioxetine after administration of single rising doses to men and multiple doses to men and women; study 2 evaluated vortioxetine pharmacokinetics in elderly adults; and study 3 assessed food effects on vortioxetine pharmacokinetics in healthy men. The primary end points included pharmacokinetic parameters of vortioxetine and incidence of adverse events (AEs). Across all studies, 130 participants were randomized and 128 participants completed the studies. Vortioxetine was absorbed and eliminated from plasma slowly, and exposure to vortioxetine increased in an almost dose-proportional manner. No clinically significant differences in the pharmacokinetics of vortioxetine or its metabolites were observed between the sexes in young and elderly adults. Study 3 demonstrated that vortioxetine and its metabolites had similar pharmacokinetics when administered in the fasted and fed states. Importantly, vortioxetine was safe and tolerated, with incidence of AEs comparable to that of placebo. No deaths or serious AEs leading to trial discontinuation were observed. Overall, vortioxetine pharmacokinetics, safety, and tolerability in Japanese adults were comparable to reports in non-Japanese populations.
三项 I 期随机、单中心研究评估了单剂量和多剂量给药后健康日本成年人中文拉法辛的药代动力学、安全性和耐受性。研究 1 评估了男性单次递增剂量和男性及女性多次剂量给药后文拉法辛的药代动力学;研究 2 评估了老年患者的文拉法辛药代动力学;研究 3 评估了食物对健康男性中文拉法辛药代动力学的影响。主要终点包括文拉法辛的药代动力学参数和不良事件(AE)的发生率。在所有研究中,共有 130 名参与者被随机分组,128 名参与者完成了研究。文拉法辛从血浆中缓慢吸收和消除,暴露量呈几乎与剂量成比例增加。在年轻和老年成年人中,文拉法辛及其代谢物的药代动力学在性别之间无临床显著差异。研究 3 表明,文拉法辛及其代谢物在空腹和进食状态下具有相似的药代动力学。重要的是,文拉法辛安全且耐受良好,AE 发生率与安慰剂相当。未观察到死亡或导致试验终止的严重 AE。总体而言,文拉法辛在日本成年人中的药代动力学、安全性和耐受性与非日本人群的报告相似。